meclinertant [Ligand Id: 1582] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL506981 (Meclinertant, Reminertant, Sr48692, SR-48692) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| NTS1 receptor/Neurotensin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989] | ||||||||
| ChEMBL | Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 F136A mutant expressed in HEK293 cells | B | 7.48 | pKd | 33 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| ChEMBL | Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 W129A mutant expressed in HEK293 cells | B | 7.57 | pKd | 27 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| ChEMBL | Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 W134A mutant expressed in HEK293 cells | B | 7.64 | pKd | 23 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| ChEMBL | Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 F127A mutant expressed in HEK293 cells | B | 7.72 | pKd | 19 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| ChEMBL | Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 P133A mutant expressed in HEK293 cells | B | 8.04 | pKd | 9.2 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| ChEMBL | Displacement of [3H]SR48692 from wild type human NTR1 expressed in HEK293 cells | B | 8.05 | pKd | 8.9 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| ChEMBL | Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 H131A mutant expressed in HEK293 cells | B | 8.08 | pKd | 8.4 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - | Mol Pharmacol (2001) 60: 1392-8 [PMID:11723247] |
| ChEMBL | Antagonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as inhibition of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay | F | 7.09 | pIC50 | 82 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3974-3978 [PMID:24997685] |
| GtoPdb | - | - | 8.2 | pIC50 | 6.31 | nM | IC50 | J Pharmacol Exp Ther (1997) 280: 802-12 [PMID:9023294] |
| ChEMBL | Displacement of [125I]I-Tyr(3)NT from human NTR1 | B | 9 | pIC50 | 0.99 | nM | IC50 | J Med Chem (2009) 52: 1803-1813 [PMID:19290594] |
| ChEMBL | Agonist activity at NTR1 in human U2OS cells after 1 hr by beta-arrestin GFP reporter gene assay | B | 4.51 | pEC50 | 31000 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 262-267 [PMID:24332089] |
| NTS1 receptor/Neurotensin receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3027] [GtoPdb: 309] [UniProtKB: P20789] | ||||||||
| ChEMBL | Displacement of [125I]NT from rat NTR1 transfected in mouse LTK cells | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem (2013) 21: 4378-4387 [PMID:23721919] |
| GtoPdb | - | - | 8.6 | pKi | - | - | - |
Mol Pharmacol (1995) 47: 1050-6 [PMID:7746272]; J Biol Chem (1998) 273: 16351-7 [PMID:9632698] |
| ChEMBL | Displacement of [125I]neurotensin from rat brain NTR1 | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (2019) 62: 8357-8363 [PMID:31390201] |
| NTS2 receptor/Neurotensin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2514] [GtoPdb: 310] [UniProtKB: O95665] | ||||||||
| ChEMBL | Binding affinity to NTR2 (unknown origin) | B | 6.38 | pKi | 418 | nM | Ki | Bioorg Med Chem (2013) 21: 4378-4387 [PMID:23721919] |
| GtoPdb | - | - | 6.4 | pKi | - | - | - | Mol Pharmacol (2001) 60: 1392-8 [PMID:11723247] |
| NTS2 receptor in Mouse [GtoPdb: 310] [UniProtKB: P70310] | ||||||||
| GtoPdb | - | - | 7.1 | pIC50 | - | - | - | Biochem Biophys Res Commun (1998) 243: 585-90 [PMID:9480852] |
| NTS2 receptor/Neurotensin receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5106] [GtoPdb: 310] [UniProtKB: Q63384] | ||||||||
| ChEMBL | Displacement of [125I]NT at rat NTS2 overexpressed in CHOK1 cells after 30 mins by gamma counting | B | 7.21 | pKi | 62 | nM | Ki | J Med Chem (2014) 57: 5318-5332 [PMID:24856674] |
| ChEMBL | Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay | F | 6.92 | pEC50 | 120 | nM | EC50 | J Med Chem (2014) 57: 5318-5332 [PMID:24856674] |
| Neurotensin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3091] [UniProtKB: Q99523] | ||||||||
| ChEMBL | Binding affinity to NTR3 (unknown origin) | B | 6.62 | pIC50 | 238 | nM | IC50 | Bioorg Med Chem (2013) 21: 4378-4387 [PMID:23721919] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
